Allapinin, tablets 25 mg 30 pcs

Allapinin is a class I C antiarrhythmic drug. It blocks fast sodium channels of cardiomyocyte membranes. It causes delay in AV and intraventricular conduction, shortens effective and functional refractory periods of atria, AV node, Gis bundle and Purkinje fibers, does not influence QT interval duration, conduction along AV node in anterograde direction, HR, BP, myocardial contractility (in initial absence of cardiac insufficiency).

It does not inhibit sinus node automatism. It does not cause negative inotropic and hypotensive effect.

Allapinin® has moderate antispasmodic, coronary dilator, choline blocker, local anesthetic and sedative effects. When administered orally the effect occurs within 40-60 minutes and maximum effect is reached after 80 minutes and lasts for 8 hours and more.

Pharmacokinetics:

Eabsorption
Bioavailability is 40%. The drug is subjected to the effect of “first passage” through the liver.
Distribution and metabolism
When administered orally, Vd is 690 L. It penetrates through the BBB.
Excretion
T1/2 is 1-1.2 h. It is eliminated by the kidneys.

Pharmacokinetics in special clinical cases

In prolonged use, increased T1/2 is possible. In chronic renal failure T1/2 is increased by 2-3 times, in liver cirrhosis by 3-10 times.

Indications

Heart palpitations, Arrhythmia, Heart pain

– supraventricular extrasystole;
– ventricular extrasystole;
– paroxysms of atrial fibrillation and flutter;
– paroxysmal supraventricular tachycardia (including WPW syndrome).Paroxysmal supraventricular tachycardia (including in WPW syndrome);
– Paroxysmal ventricular tachycardia (in the absence of organic heart disease).

Active ingredient

Lappaconitine hydrobromide

Composition

1 tablet contains:

• Active substance:
• allapinin – 25 mg;
• Auxiliary substances:
• sucrose (sugar),
• potato starch,
• calcium stearate (calcium stearate).

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How to take, the dosage

Allapinin is administered orally at 25 mg (1 tablet) every 8 hours, if there is no therapeutic effect – every 6 hours.

The single dose may be increased to 50 mg (2 tablets) every 6-8 hours. The maximum daily dose is 300 mg (12 tablets).

The duration of treatment and changes in dosing regimen (dose increases) are determined by the physician.

The drug is taken orally, after eating, with a small amount of water at room temperature; do not crush the tablets.

Interaction

In concomitant use of Allapininf with inducers of microsomal liver enzymes, the effectiveness of lappaconitine hydrobromide is reduced, the risk of toxic effects increases.

The antiarrhythmic agents of other classes increase the risk of arrhythmogenic effects.

Lappaconitine hydrobromide increases the effect of nondepolarizing myorelaxants.

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Special Instructions

Before initiating Allapinin® administration, water-electrolyte metabolism disorders should be corrected; during therapy, water-electrolyte balance control is necessary.

In patients who have had an acute myocardial infarction or in patients with heart failure, as well as in patients with an artificial heart pacemaker installed, its stimulation threshold may increase.

The dose of Allapinin® should be reduced if headache, dizziness, or diplopia develop.

If sinus tachycardia occurs with prolonged use of the drug, low-dose beta-adrenoblockers should be used.
1 tablet contains 74 mg of carbohydrates, which corresponds to 0.01 USE.

Impact on driving and operating machinery

When using the drug, caution must be taken when performing potentially hazardous activities requiring particular attention and quick reactions (driving, operating moving machinery).

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Contraindications

– sinoatrial block;
– AV-blockade of II and III degree (without artificial pacemaker);
– cardiogenic shock;
– right bundle branch block combined with a left bundle branch block;
– severe arterial hypotension (systolic BP less than 90 mm Hg).Systolic BP less than 90 mm Hg);
– moderate and severe chronic cardiac insufficiency III-IV functional class according to NYHA classification;
– significant left ventricular myocardial hypertrophy (≥1.4 cm);
– presence of postinfarction cardiosclerosis;
– severe liver and/or kidney function disorders;
– fructose intolerance, glucose/galactose malabsorption syndrome, sucrose/isomaltase deficiency (the preparation contains sucrose);
– childhood and adolescence under 18 years of age (efficacy and safety have not been established);
– hypersensitivity to the drug Allapinin.

. The preparation should be used with caution in case of 1st degree AV-blockade, intraventricular conduction disorders, VSU, bradycardia, severe disorders of peripheral circulation, closed-angle glaucoma, prostatic hypertrophy, Purkinje conductivity disorder, Gis bundle leg block, electrolyte metabolism disorders (hypokalemia, hyperkalemia, hypomagnesemia), concomitant use with other antiarrhythmic drugs.

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Side effects

CNS and peripheral nervous system disorders: dizziness, headache, sensation of heaviness in the head, ataxia, diplopia are possible.

Cardiovascular system disorders: possible AV and intraventricular conduction disorders, sinus tachycardia (with long-term use), arrhythmogenic effect, ECG changes (PQ interval prolongation, QRS complex expansion).

Others: skin hyperemia and allergic reactions are possible.

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Overdose

Symptoms: the drug has a low therapeutic latitude; therefore, severe intoxication may easily occur (especially with the simultaneous use of other antiarrhythmic agents): prolongation of PR and QT intervals, expansion of the QRS complex, increased amplitude of the T wave, bradycardia, sinoatrial blockade, AV blockade, asystole, paroxysms of polymorphic ventricular tachycardia, reduced myocardial contractility, marked BP decrease, dizziness, blurred vision, headache, gastrointestinal disturbances.

Treatment: symptomatic therapy is carried out.

To treat ventricular tachycardia, class I A and I C antiarrhythmic drugs should not be used. Sodium hydrogen carbonate can eliminate QRS complex dilation, bradycardia and arterial hypotension.

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Similarities

Allaforte